PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 10660118-1 2000 The site of interaction for the 1-(3",4",5"-trimethoxybenzyl) group of trimetoquinol (TMQ) with beta-adrenoceptors (beta-ARs) is important for the rational design of highly potent and beta3-AR-selective analogs. Tretoquinol 71-84 adrenoceptor beta 3 Homo sapiens 184-192 11150922-4 2001 The 3",5"-diiodo-4"-amino analog of TMQ was the most potent beta(3)-AR agonist, 17-fold more potent at the beta(3)-AR versus the beta(1)-AR. Tretoquinol 36-39 adrenoceptor beta 3 Homo sapiens 60-70 11150922-4 2001 The 3",5"-diiodo-4"-amino analog of TMQ was the most potent beta(3)-AR agonist, 17-fold more potent at the beta(3)-AR versus the beta(1)-AR. Tretoquinol 36-39 adrenoceptor beta 3 Homo sapiens 107-117 11150922-5 2001 Masking of the 6,7-dihydroxy group of the catechol ring of 3",5"-diiodo-4"-acetamido analog of TMQ, a potent beta(1)- and beta(3)-AR agonist, abolished activity at both beta-AR subtypes. Tretoquinol 95-98 adrenoceptor beta 3 Homo sapiens 122-132 11150922-6 2001 Furthermore, substitution of a strong electron withdrawing group such as the trifluoromethyl moiety at the 1-benzyl ring of TMQ dramatically decreased potency at beta(1)- and beta(3)-AR compared to TMQ. Tretoquinol 124-127 adrenoceptor beta 3 Homo sapiens 175-185 11150922-8 2001 Our results define the structural and electronic properties of substituents on TMQ necessary for potent activation of beta(1)- and beta(3)-AR and suggest that further modifications of the 1-benzyl iodine-substituted analogs may yield potent beta(3)-AR agonists. Tretoquinol 79-82 adrenoceptor beta 3 Homo sapiens 131-141 11150922-8 2001 Our results define the structural and electronic properties of substituents on TMQ necessary for potent activation of beta(1)- and beta(3)-AR and suggest that further modifications of the 1-benzyl iodine-substituted analogs may yield potent beta(3)-AR agonists. Tretoquinol 79-82 adrenoceptor beta 3 Homo sapiens 241-251 10660118-1 2000 The site of interaction for the 1-(3",4",5"-trimethoxybenzyl) group of trimetoquinol (TMQ) with beta-adrenoceptors (beta-ARs) is important for the rational design of highly potent and beta3-AR-selective analogs. Tretoquinol 86-89 adrenoceptor beta 3 Homo sapiens 184-192 10660118-4 2000 A similar rank order of binding affinities (K(i) approximately 0.11 to 2.5 microM) and potencies (K(act) approximately 0.45 to 9.5 nM) was obtained for TMQ analogs on the human beta3-AR. Tretoquinol 152-155 adrenoceptor beta 3 Homo sapiens 177-185 10660118-9 2000 Thus, the lipophilic 1-benzyl ring of TMQ analogs interacts with a hydrophobic region of the beta-AR that may represent an exo-site or an allosteric binding site. Tretoquinol 38-41 adrenoceptor beta 3 Homo sapiens 93-100 10691685-1 2000 Trimetoquinol (1, TMQ) is a potent nonselective beta-adrenergic receptor (AR) agonist and a thromboxane A(2)/prostaglandin endoperoxide (TP) receptor antagonist, while 3",5"-diiodo-TMQ (2) exhibits beta(3)-AR selectivity. Tretoquinol 0-13 adrenoceptor beta 3 Homo sapiens 198-208 10377236-2 1999 Replacement of the catechol moiety of TMQ with a 2-aminothiazole group resulted in novel thiazolopyridine derivatives 9-11 which have been synthesized and evaluated for biological activity on human beta1-, beta2-, and beta3-AR. Tretoquinol 38-41 adrenoceptor beta 3 Homo sapiens 218-226 10525112-2 1999 In cAMP accumulation assays, (-)-TMQ was 214-, 281-, and 776-fold more potent than (+)-TMQ at stimulating beta(1)-, beta(2)-, and beta(3)-adrenoceptor subtypes, respectively. Tretoquinol 29-36 adrenoceptor beta 3 Homo sapiens 116-150 10525112-2 1999 In cAMP accumulation assays, (-)-TMQ was 214-, 281-, and 776-fold more potent than (+)-TMQ at stimulating beta(1)-, beta(2)-, and beta(3)-adrenoceptor subtypes, respectively. Tretoquinol 83-90 adrenoceptor beta 3 Homo sapiens 116-150 10525112-3 1999 In radioligand binding assays, (-)-TMQ exhibited 123-, 331-, and 5-fold greater affinity than (+)-TMQ for beta(1)-, beta(2)-, and beta(3)-adrenoceptor subtypes, respectively. Tretoquinol 31-38 adrenoceptor beta 3 Homo sapiens 116-150 10525112-3 1999 In radioligand binding assays, (-)-TMQ exhibited 123-, 331-, and 5-fold greater affinity than (+)-TMQ for beta(1)-, beta(2)-, and beta(3)-adrenoceptor subtypes, respectively. Tretoquinol 94-101 adrenoceptor beta 3 Homo sapiens 116-150 10525112-4 1999 (-)-TMQ and (+/-)-TMQ activated the human beta(3)-adrenoceptor with an 8.2- and 3.4-fold greater efficacy, respectively, than the reference beta-adrenoceptor agonist (-)-isoproterenol (efficacy = 1). Tretoquinol 0-7 adrenoceptor beta 3 Homo sapiens 42-62 10525112-4 1999 (-)-TMQ and (+/-)-TMQ activated the human beta(3)-adrenoceptor with an 8.2- and 3.4-fold greater efficacy, respectively, than the reference beta-adrenoceptor agonist (-)-isoproterenol (efficacy = 1). Tretoquinol 12-21 adrenoceptor beta 3 Homo sapiens 42-62 10525112-5 1999 The 3",5"-diiodo analogs of TMQ were partial agonists of the beta(2)-adrenoceptor relative to (-)-isoproterenol, and their potencies were 5- to 10-fold higher at the beta(3)-adrenoceptor as compared with beta(1)-adrenoceptors. Tretoquinol 28-31 adrenoceptor beta 3 Homo sapiens 166-186 10525112-7 1999 Furthermore, the 3",5"-diiodo-4"-methoxybenzylTHP derivative of TMQ was 65-fold more potent than the corresponding 3",4",5"-trimethoxybenzylTHP at the human beta(3)-adrenoceptor. Tretoquinol 64-67 adrenoceptor beta 3 Homo sapiens 157-177 10525112-8 1999 Our results indicate that 6, 7-dihydroxy-catechol-modified and 1-benzyl halogen-substituted derivatives of TMQ represent promising leads for the development of beta(3)-adrenoceptor-selective agonists. Tretoquinol 107-110 adrenoceptor beta 3 Homo sapiens 160-180